| Assay Method Information | |
| | In Vitro Assay (Protocol 2) |
| Description: | Compounds of Formula (I), were diluted in eight concentrations in the extracellular solution composed of physiological saline, buffered with HEPES (mM): NaCl, 137; KCl, 4; CaCl2, 3.8; MgCl2, 1; HEPES, 10; Glucose, 10; pH 7.4. The extracellular solution is composed of (mM) CsCl, 50; CsF, 90; MgCl2, 5; EGTA, 5; HEPES, 10; pH 7.2. The duration of exposure of each compound with the cells expressing Nav 1.7 or Nav 1.8 was at least five minutes and the assays were performed at room temperature.The measurements of the sodium currents of Nav 1.8 and Nav 1.7 were obtained using the voltage protocols described below: A holding voltage of-100 mV was established followed by an inactivation voltage step at −40 mV for 8 seconds, followed by a −100 mV step for 20 ms, followed by a 20 ms step for 10 mV for Nav 1.8 or 0 mV for Nav 1.7 (TP1A) before returning to the holding voltage of-100 mV. Protocols were repeated at a frequency of 0.05 Hz and current amplitude was quantified over the TP1A phase log. |
| Affinity data for this assay | |
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